Synthesis and Evaluation of Antimicrobial Activity of N-Substituted Indole Derivatives and Molecular Docking Studies DOI
Ashish Ranjan Dwivedi, Vijay Kumar,

Neha Neha

et al.

Current Organic Chemistry, Journal Year: 2022, Volume and Issue: 26(16), P. 1565 - 1574

Published: Aug. 1, 2022

Abstracts: The increasing burden of microbial infection and emerging resistance against the available antimicrobial drugs drives development new agents. Two different series indole-based compounds (VN-1 to VN-18) were synthesized analyzed for activity by calculating diameter inhibition zone using broth dilution method well diffusion Escherichia coli (E. coli) environmental microbes. Most displayed good moderate E. coli, VN-4 VN-9 inhibitory tested Molecular docking binding energy calculation studies all have been performed targeting FabI, where most showed significant interactions with aromatic nicotinamide moiety NAD+. In molecular dynamics studies, stays inside cavity sufficient time induce activity. Thus, these derivatives may lead agents that act as FabI inhibitors.

Language: Английский

Recent studies of nitrogen containing heterocyclic compounds as novel antiviral agents: A review DOI
Arif Mermer, Turgut Keleş, Yakup Şirin

et al.

Bioorganic Chemistry, Journal Year: 2021, Volume and Issue: 114, P. 105076 - 105076

Published: June 10, 2021

Language: Английский

Citations

265
Recent progress in biologically active indole hybrids: a mini review DOI

Esraa Mahmoud,

Alaa M. Hayallah,

Suzana Kovacic

et al.

Pharmacological Reports, Journal Year: 2022, Volume and Issue: 74(4), P. 570 - 582

Published: May 20, 2022

Language: Английский

Citations

63
Synthesis and biological activity of new indole based derivatives as potent anticancer, antioxidant and antimicrobial agents DOI
Metin Konuş, Doğan Çetin,

Nurhan Didem Kızılkan

et al.

Journal of Molecular Structure, Journal Year: 2022, Volume and Issue: 1263, P. 133168 - 133168

Published: April 27, 2022

Language: Английский

Citations

34
Indole/isatin‐containing hybrids as potential antibacterial agents DOI

Feng Song,

Zhenghua Li, Yunqiang Bian

et al.

Archiv der Pharmazie, Journal Year: 2020, Volume and Issue: 353(10)

Published: July 15, 2020

Abstract The emergence and worldwide spread of drug‐resistant bacteria have already posed a serious threat to human life, creating the urgent need develop potent novel antibacterial drug candidates with high efficacy. Indole isatin (indole‐2,3‐dione) present wide structural mechanistic diversity, so their derivatives possess various pharmacological properties occupy salient place in development new drugs. Indole/isatin‐containing hybrids, which demonstrate promising activity against panel clinically important Gram‐positive Gram‐negative bacteria, are privileged scaffolds for discovery candidates. This review, covering articles published between January 2015 May 2020, focuses on structure–activity relationship (SAR) indole/isatin‐containing hybrids potential application fighting bacterial infections, facilitate further rational design

Language: Английский

Citations

44
Thiophene‐containing compounds with antimicrobial activity DOI
Gheorghe Roman

Archiv der Pharmazie, Journal Year: 2022, Volume and Issue: 355(6)

Published: March 15, 2022

Thiophene, as a member of the group five-membered heterocycles containing one heteroatom, is simplest heterocyclic systems. Many synthetic strategies allow accurate positioning various functionalities onto thiophene ring. This review provides comprehensive, systematic and detailed account developments in field antimicrobial compounds featuring at least ring their structure, over last decade.

Language: Английский

Citations

27
Synthesis, design, and assessment of novel morpholine-derived Mannich bases as multifunctional agents for the potential enzyme inhibitory properties including docking study DOI

Songül Boy,

Fikret Türkan, Murat Beytur

et al.

Bioorganic Chemistry, Journal Year: 2020, Volume and Issue: 107, P. 104524 - 104524

Published: Dec. 4, 2020

Language: Английский

Citations

33
2-methylindole analogs as cholinesterases and glutathione S-transferase inhibitors: Synthesis, biological evaluation, molecular docking, and pharmacokinetic studies DOI Creative Commons
Adnan Çetin, Ercan Bursal, Fikret Türkan

et al.

Arabian Journal of Chemistry, Journal Year: 2021, Volume and Issue: 14(12), P. 103449 - 103449

Published: Sept. 22, 2021

• 2-methylindole analogs were designed, synthesized and characterized. The target ( 4a–4j ) evaluated for their inhibitory potential against glutathione S-transferase (GST), acetylcholinesterase (AChE), butyrylcholinesterase (BChE) activities. Molecular docking studies conducted to correlate the in vitro results identify possible mode of interactions at active pocket site receptors. pharmacokinetic carried out using SwissADMET analyses. In this study, we aimed (i) synthesize new containing various amino structures, pyrrolidine, piperidine, morpholine, substituted phenyl groups through structural molecular modifications, (ii) evaluate pharmaceutical via assessing enzyme activity (BChE), (iii) predict ADMET properties analogs, (iv) reveal between with GST, AChE, BChE enzymes several software. inhibition assays showed that indole exhibited moderate good activities enzymes. Briefly, 4b 4i 4a BChE, 1 GST detected be higher or close standard inhibitor compounds. analog was have best both AChE lowest IC 50 values as 0.648 µM 0.745 BChE. analyses relationship could help design inhibitors cholinergic pathways based on derivatives.

Language: Английский

Citations

31
Cytotoxic Activity, Anti-migration and in silico Study of o-Coumaric acid on H1975 Non-small Cell Lung Cancer Cells DOI Open Access
Doğukan Mutlu

Cumhuriyet Science Journal, Journal Year: 2025, Volume and Issue: 46(1), P. 35 - 40

Published: March 25, 2025

Lung cancer represents the most common malignancy and remains primary cause of cancer-related deaths worldwide. Phenolic acids, including o-coumaric acid (OCA), have attracted considerable attention due to their diverse biological activities, particularly anticancer properties. This study evaluates cytotoxic activity OCA, along with its anti-migration effects molecular docking analysis. The in vitro cytotoxicity OCA on H1975 cells was assessed using MTT assay Acridine orange/ethidium bromide (AO/EB) staining, while impact cell migration analyzed through an scratch assay. demonstrated against cells, IC50 value 8.107 mM, inhibited by 38%. Additionally, silico performed investigate interaction epidermal growth factor receptor (EGFR). Although exhibited notable binding interactions EGFR, hydrogen bonding pi-alkyl interactions, affinity (−5.9 kcal/mol) lower compared Gefitinib (−8.5 kcal/mol), a known EGFR inhibitor. These findings suggest that holds potential as therapeutic agent non-small lung cancer, efficacy may be enhanced structural modifications, synthesis derivatives, warranting further research into industrial clinical applications

Language: Английский

Citations

0
Synthetic approaches, emerging applications, and challenges of indole-based five-membered heterocycles in medicinal chemistry DOI Creative Commons

M. Padmapriya,

Sushruta S. Hakkimane, Santosh L. Gaonkar

et al.

Deleted Journal, Journal Year: 2025, Volume and Issue: 7(3)

Published: March 7, 2025

Abstract Scientists are fascinated by the indole structure due to its diverse biological activities, encompassing both itself and numerous substituted derivatives. Heterocycles, particularly those containing indoles, play pivotal roles in domains of medicinal chemistry, drug designing discovery, agrochemicals, photochemistry, dyes, other applications, which has led their prominence chemistry field. This review highlights applications indole-based five-membered heterocycles as versatile scaffolds for development, emphasizing therapeutic potential antidiabetic, anti-inflammatory, anticancer, antimicrobial, antioxidant agents, antialzheimer anticonvulsant agents. A comprehensive literature search was carried out explore chemical, biological, structural activity correlations hybrids. Studies published between 2017 2024 were chosen from databases such PubMed, Scopus Google Scholar, synthesis, application chemistry. Unique this is exploration structure–activity relationships (SAR), synthetic approaches emerging challenges development drugs. Key insights include innovative strategies enhance efficacy through modifications various derivatives areas. These findings hold great improving design more effective pharmaceuticals. Graphical abstract

Language: Английский

Citations

0
Design, synthesis, and antiproliferative activity of new indole/1,2,4‐triazole/chalcone hybrids as EGFR and/or c‐MET inhibitors DOI Creative Commons

Esraa Mahmoud,

Dalia Abdelhamid, Bahaa G. M. Youssif

et al.

Archiv der Pharmazie, Journal Year: 2024, Volume and Issue: 357(9)

Published: June 21, 2024

A novel group of indolyl-1,2,4-triazole-chalcone hybrids was designed, synthesized, and assessed for their anticancer activity. The synthesized compounds exhibited significant antiproliferative Compounds 9a 9e cancer inhibition with GI

Language: Английский

Citations

3